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Transgender

Explore our Transgender category, featuring a range of products tailored to assist with hormone replacement therapy for transgenders. We provide feminizing products, including female hormones and male hormone antagonists, designed to support transgender individuals in their journey. Our offerings extend to solutions for reducing facial hair, specifically catering to male-to-female transsexuals.

Browse through different classes of medication for transgender hormone therapy listed on the left side of the page. Click on a specific class to reveal principal brand name products in the left column and generic alternatives on the right. Use the search feature to find the transgender drug or product you are looking for by entering the active ingredient, e.g. Dutasteride, or the product name, e.g. Duprost.

Our Anti-Androgens class of Transgender drugs contains products that are used to block the actions of testosterone and reduce the effects of male hormones during a gender reassignment programme. These include Siterone and Spiractin.

What is an androgen?

Androgen is a generic term for male hormones which are steroid hormones that bind to the androgen receptor and control the development of male characteristics.  The main androgen is testosterone, which is converted to its active and more potent metabolite dihydrotestosterone (DHT) by the action of the enzyme 5-alpha reductase and.  Both testosterone and DHT bind to the androgen receptor within responsive cells of various tissues including brain, bone, hair follicles, testes and prostate cells.  

What is an anti-androgen?

Anti-androgens are drugs that counteract or block the biological effects of the male hormone testosterone or its active metabolite DHT on a wide range of tissues where they normally have biological activity.  They are usually steroidal and fat soluble and pass through the cell membrane to interact with the androgen steroid receptors inside the cell and compete with testosterone or DHT for these receptors.  This blocks expression of genes involved in the development and maintenance of male characteristics. 

Some anti-androgens are non-steroidal and also compete with testosterone and DHT for receptor binding, thereby blocking the action of testosterone and also the production of testosterone by the testes.  Other non-steroidal anti-androgens inhibit the conversion of DHT from testosterone.  Some drugs have anti-androgenic activity as a side effect. 

Products for blocking the action of androgens

  • Dutasteride and Finasteride are 5α-reductase inhibitors and work by inhibiting the action of the enzyme type II 5α-reductase, which converts the male hormone testosterone to DHT
  • Flutamide is a non-steroidal anti-androgen that blocks the action of androgens by binding to same receptor but has no steroid effects
  • Bicalutamide is a non-steroidal anti-androgen
  • Cyproterone is a steroidal anti-androgen
  • Spironolactone is a synthetic steroid which is primarily a diuretic but has anti-androgenic activity as a side effect and works by by decreasing androgen production 
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Our Estrogens class of products contains transgender hormone pills, particularly various forms of the female hormone estrogen such as Estrofem and Progynova. Use these in a feminizing regimen for transgender hormone therapy during a gender reassignment programme.

About estrogen

Estrogens are produced by the ovaries along with progesterone at certain stages of the menstrual cycle and their production is under control of follicle stimulating hormone (FSH) and luteunising hormone (LH) produced by the pituitary gland, which are in turn under the control of gonadotrophin releasing hormones produced by the hypothalamus in the brain.  

Estrogen is the main female hormone that stimulates development of female secondary sexual characteristics like breast development, body shape and regulating the menstrual cycle.  Therefore, estrogen is used as the main component of trangender hormone therapy for male to female transexuals while at the same time overriding the effects of testosterone.  

Different forms of estrogen

Estrogen exists in several forms and with different potencies:

  • Estradiol, specifically 17-beta-estradiol or E2, is the major and most active form of natural estrogen in the body produced by the ovaries and is responsible for the main actions of estrogen
  • Ethinyloestradiol is a synthetic form of 17-beta-estradiol that is more resistant to metabolism in the liver than natural estradiol but has the same biological activity. 
  • oestradiol valerate is a prodrug (or precursor) of natural human oestradiol and is converted to 17-beta-estradiol by esterase enzymes in the blood and liver.  It is an effective form of estrogen used for intramuscular administration (injection) as it is absorbed slowly and lasts longer that estradiol itself. 
  • Estrone or E1 becomes the most prominent form of natural estrogen during menopause, as estradiol drops, and is produced primarily in the adrenal glands.  Estrone is readily converted into a long lasting form estrone sulphate which concentrates in breast tissue of post-menopausal women and is thought to be involved the development of breast cancer, by being converted to estradiol.  
  • Estriol or E3 is the weakest of the three natural forms of oestrogen.  It is the prominent form of estogen during pregnancy and is produced by the placenta, but plays no significant role in non-pregnant women as it is mild, short acting and normally present in small amounts.
  • Conjugated oestrogens are a mixture of several different forms of estrogen (at least 10) isolated from horse urine.  They contain mainly forms of estrogen that are in the sulphate form and can be easily absorbed and converted to the active form estradiol.

Delivery methods for estrogens

Estrogen hormone replacement therapy is available in several different preparations and routes of administration.  These include:

  • Oral preparations which are subjected to metabolism by the liver and is associated with side effects, such as painful swollen breasts, nausea, headache.
  • Skin patches allow oestrogen to diffuse through the skin and into the blood and allows for lower doses to be used, as estrogen bypasses liver and is therefore, not subject to first pass metabolism by the liver.  It also provides more constant blood levels as it diffuses into the blood at a steady rate
  • Topical transdermal creams and gels which are rubbed into the skin so that the estrogen diffused through the skin directly into the blood circulation, allowing the estrogen to be released slowly through the skin. 

Products available for estrogen hormonal therapy

The most commonly used estrogens as part of a feminising regime for transgender hormone therapy are the more potent forms of estrogen including estradiol (17-beta-estradiol), oestradiol valerate and conjugated oestrogens.  Estriol can also be used but is less effective.

  • estradiol for oral administration, skin patch or injection
  • oestriol for oral administration
  • conjugated oestrogens for oral administration
  • oestradiol valerate for injection
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Our Facial Hair Reduction class of Transgender products contains Eflora Cream for removing unwanted facial hair. Use it in a feminizing regimen during a male-to-female gender reassignment programme. 

Hormonal control of hair development

Androgen hormones are responsible for secondary sexual characteristics in men, including facial hair growth.  Androgens regulate the hair follicles and at puberty transform them from vellus follicles that produce the tiny almost invisible hairs that cover both male the and female body into the larger terminal follicles, producing pigmented hairs typical of the male facial hair, as well as chest hair and other body hair.  Androgens, particularly the active metabolite of testosterone dihydrotestosterone (DHT) also inhibit hair in other parts of the body, such as on the scalp by causing the terminal follicles to regress to vellus follicles, causing male pattern baldness or androgenic alopecia.

Use of anti-androgens as part of a feminising regime will reduce the amount and type facial hair, but may not eliminate it altogether.  

The hair growth cycle and its regulation

Hair goes through a 3-stage growth cycle.  The anagen phase, which is the active growth phase, catagen, where the hair stops growing and shrinks, before being shed during the telogen phase, to be replaced by a new hair.

The enzyme ornithine decarboxylase is an important rate limiting enzyme required the biosynthesis of certain proteins required for hair growth and is found in high levels in the hair follicles during the anagen phase of the hair growth cycle.  The levels of this enzyme then drop as the hair follicle enters the catagen phase.  Ornithine decarboxylase is also important in cell division and cell proliferation and actively growing hairs undergo rapid cell division. 

Blocking hair growth

Eflornithine is a drug that binds to ornithine decarboxylase and inhibits its activity. This action of ornithine decarboxylase can be used to block the growth and cell division of the terminal hair follicles that produce facial hair.  It is available as a topical cream and can help slow down the production of facial hair during the feminisation programme but it does not destroy the hair or prevent it from growing back.  
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Our Progestins class of Transgender products contain various forms of the female hormone progesterone. Synthetic progestins and progestogens such as progesterone Endogest Progestin or Provera are used in a feminizing regimen for transgender hormone therapy during a gender reassignment programme. 

What are progestins and progestogens?

Progesterone is the female hormone that in women prepares the endometrium (lining of the uterus) for a potential pregnancy.  Progestogens have the same biological activity as naturally occurring progesterone but the chemical structure has been slightly altered to improve stability and absorption. Progestins are synthetic progestogens that have a different chemical structure to progesterone but similar biological effects. 

Progestins and progestogens are used medically for contraception, hormone replacement therapy in menopausal women and to treat certain conditions like endometriosis.  

Use of progestins and progestogens for transgender hormone therapy

Although the clinical opinion is mixed on their effectiveness of use, progestins and progestogens can be used as part of the feminization regime for male to female transgender hormone therapy1.  The rational for this is that adding progesterone in some form more closely simulates the female hormone cycle.  However, there are also some side effects including, weight gain, oedema, and mood swings.  There is also an increased risk of developing breast cancer2.

Progesterone suppresses testosterone production and is also thought to support breast development in transgender hormone therapy, which is one of the roles of progesterone in females.  Although oestrogen is primarily responsible for breast development in females, progesterone is involved in regulation the growth and differentiation of breast tissue.  Also during pregnancy, progesterone contributes to increasing the size of breasts and the nipples in preparation for lactation. 

Progestin products

Progestins, which are synthetic progestogens, available are:

  • Medroxyprogesterone
  • Hydroxyprogesterone
  • Dydrogesterone
Medroxyprogesterone and hydroxyprogesterone are both administered by injection and are more potent and longer-acting than natural progesterone. Medroxyprogesterone is also available for oral administration as is dydrogesterone.  Progestins are more active when taken orally than natural progesterone and do not have other hormonal effects.

Progestogen products

Micronized progesterone, in which natural progesterone is reduced to tiny particles for better absorption, is available as a gel and as capsules.

Progesterone is also available for injection in an oil base for stability. 

References

  1. Wierckx K, Gooren L, T'Sjoen G. Clinical review: Breast development in trans women receiving cross-sex hormones. J Sex Med 2014 May;11(5):1240-7
  2. Axlund SD, Sartorius CA. Progesterone regulation of stem and progenitor cells in normal and malignant breast. Mol Cell Endocrinol 2012 Jun 24;357(1-2):71-9. 



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For more transgender drugs and products, please browse our “Others” category. We provide cost-effective branded medicines and generic alternatives to support hormone replacement therapy for transgenders.

Anti-oestrogens

Anti-oestrogen medicines, such as tamoxifen and anastrozole, are used to treat breast cancer in women.  They can also be used to support the gender reassignment process for female to male transgender patients.  Anastrozole blocks the synthesis of oestrogen in peripheral tissues such as adrenal glands and fat tissue, where testosterone can be converted to oestrogen.  Tamoxifen blocks activation of the oestrogen receptor, preventing stimulation of female secondary sexual characteristics like breast tissue.  Both medications help reduce the amount of oestrogen, which supports the suppression of female characteristics and the increase in masculine characteristics.

Combination products

Combining medications that promote female characteristics while suppressing male characteristics, can help with the male to female gender reassignment process.

Medications combining oestrogen with an antiandrogen like cyproterone, are used to treat conditions in women caused by overproduction of androgens.  These conditions include hirsutism (unwanted hair) and acne.  Cyproterone alone is used to control extreme sexual desire in men that can cause aggressive behaviour.  A combination of oestrogen with an antiandrogen can also be used to promote feminization while suppressing male characteristics, which helps support the gender reassignment process for male to female transgender patients.  Oestrogens promote female characteristics, such as stimulating breast development and help make changes to the male body, such as reducing muscle mass and redistributing body fat.  Antiandrogens are drugs that block the production and the effects of the male hormone testosterone and its more potent form, dihydrotestosterone (DHT).  Development of secondary male characteristics are stimulated by DHT.  These include growth of the prostate gland, the testes, and body and facial hair. 

Several forms of oestrogen can be used to promote the feminization process.  These include conjugated oestrogens, which is a mixture of natural oestrogen in different forms.  This preparation of oestrogen is used for hormone replacement therapy in women, to relieve symptoms of menopause.  Conjugated oestrogens can also be used for hormone therapy as part of the gender reassignment process in male to female patients.  Oestrogen combined with a progestogen like medroxyprogesterone, a synthetic form of the female sex hormone progesterone, may enhance the feminization process.  Progesterone is involved in breast development.  It also has antiandrogenic activity and works by blocking testosterone production.

Topical anaesthetic cream

A cream containing a combination of two topical anaesthetics is used for pain relief during minor superficial surgical procedures.  These types of surgery may be needed during the gender reassignment process, for example, surgery involving genital skin.

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For any questions about our products, please refer to our FAQ page or contact us.

What is gender?

Gender is a complex concept encompassing an individual’s identity. Initially, it was used as a way to differentiate male from female, between masculine and feminine. However, gender is not a binary — and it is not an easy word to define. There are many components to its definition, including biology, genetics, behavior patterns, activities, social identity, and psychological traits. Society associates many of these characteristics with one sex, either male or female. During the earlier decades of the 20th century, the concepts of transgenderism, gender dysphoria, or even transgender hormone therapy were still far from reality. 

However, in 1955, gender was first described in terms of sexual roles by John Money, a doctor specialising in research into the biology and psychology of gender. He also used the term gender identity for the first time in 1966 to describe a person’s subjective sense of their own sex, which may not be the same as their physical gender based on the genitals they were born with.

Then, in 1974, the term “gender dysphoria” was first used to describe the distress that can be felt by a person who is dissatisfied or discontented with the physical sexual identity they were born with or the sexual role in society that is expected of them and this is also known as gender identity disorder. Coining these terms helped deepen the understanding of transgenderism — that there are people who have a gender identity that does not match their biological sex and includes people described by the categories of transsexual or transgender. Furthermore, bringing these concepts to light paved the way for sexual transition through processes like transgender hormone therapy, allowing people to live completely in accordance with their identity.

Transgender or transsexual

A transgender describes a person who lives within their body and is not necessarily male or female, but may incorporate both male and female behavior and appearance. They usually do not wish to have genital surgery and manage their gender identity by the way they dress and how they present themselves. However, they may still want to undergo hormone replacement therapy for transgenders to develop characteristics that are more feminine or masculine, depending on their gender identity.

A transsexual is someone who has a gender identity that more closely resembles the opposite sex and they often wish to change their physical sex attributes and live completely as the opposite sex. For a transsexual, the next step would be genital surgery and transgender hormone therapy to complete the gender reassignment process.

Gender reassignment

The term gender reassignment refers to the process whereby the physical sexual characteristics are altered to reflect a person’s gender identity.  This process of change from the one gender to another, also known as transition, incorporates medical procedures, hormone replacement therapy and social changes, such as the person’s role and legally changing their name to one that better suits the opposite gender.

The genetics of gender 

Gender is determined by several factors, including hormones present during fetal development, reinforced behavior patterns as well as genetics. While genetics usually determines gender, XX being female and XY being male, there are other genetic combinations that introduce shades of gray. Some of these change the physical appearance, such as XXY, which results in male and female genitals and is known as Klinefelder’s syndrome. The genetic makeup XYY results in male genitals but can also cause various antisocial or aggressive behaviors. The genetic makeup XO or Turner’s syndrome results in a female body but behavior and personality are affected.

The role of hormones in sex and gender

Transgender hormone therapy is crucial for individuals seeking to develop more feminine or masculine characteristics, as hormones play a vital role in shaping and aligning physical attributes with their gender identity. Remember that the term “sex” refers to the biological difference between the male and female body. However, gender refers to the expected behavioural and cultural differences within society that are determined by a person’s sex. Without interventions like medical transitions, a person’s sex does not change but gender can.

The physical differences between males and females develop in response to steroid hormones, which begin influencing development before birth. All fetuses develop along female lines until testicular hormones initiate male differentiation. Although estrogen is considered the female hormone, testosterone is also present in females but in lesser amounts. It is the higher levels of testosterone in males that determine the development of male physical changes and also influence brain development, which ultimately influences behavior. At puberty, female secondary sexual characteristics are induced by estrogen and progesterone produced by the ovaries. Meanwhile, male secondary sexual characteristics are induced by androgens, particularly testosterone and its potent metabolite dihydrotestosterone or DHT produced by the testes.

Transgender hormone pills and other interventions allow individuals to induce hormonal changes that align more closely with their gender identity. These are known as feminization and masculinization regimens. At InhousePharmacy.vu, our Transgender category contains feminizing products like estrogen and anti-androgen pills. These transgender drugs work to influence body fat distribution, skin texture and breast development. Individuals desiring a more masculine appearance may be prescribed testosterone pills to promote facial and body hair growth, deepening of the voice and muscle development.

Feminization regime

Transgender hormone therapy tailored for male-to-female individuals is often referred to as feminization or a feminizing regimen. It involves a strategic approach to modify physical characteristics using transgender hormone pills. These medications suppress original male attributes by blocking male hormones while simultaneously stimulating the development of female secondary sexual characteristics using female hormones. A comprehensive feminizing programme encompasses multiple hormonal interventions, each playing a distinct role in one’s transition.

The effects of transgender hormone therapy for male-to-female individuals include:

  • redistribution of body fat to redefine body shape
  • breast development
  • reduction in appearance and coarseness of body hair
  • reduced musculature in the hands and feet
  • changes in appearance of the skin
  • reduced activity of the sebaceous glands

Overall, these changes brought about by transgender hormone pills lead to a more feminine appearance and less pronounced masculine features.

Products for feminisation hormone therapy

Feminizing hormone therapy involves a carefully curated drug regimen designed to bring about your desired physical changes. Before you purchase transgender hormone pills for feminization, it is important that you seek medical guidance throughout your journey. A licensed endocrinologist can design a feminization programme that suits your goals, while psychologists can help you cope with the emotional and social challenges that come with your transition.

When you’re ready, these are the common medications involved in transgender hormone therapy for male-to-female transitioners:

  • Estrogens — These primary female sex hormones play a pivotal role in promoting female secondary sexual characteristics, and its most potent form is estradiol. Estrogens contribute to breast development, redistribution of body fat and developing a softer skin texture.
    Estrogens can be administered in different ways: orally through transgender hormone pills; transdermally with patches, creams and gels; and through injectables.
  • Anti-androgens — These are integral to feminizing hormone therapy, aiming to reduce the effects of male hormones, especially testosterone. Anti-androgens suppress masculine characteristics, including facial hair growth, deepening the voice and high muscle mass.
  • Anti-androgens are another type of transgender drug administered in pill form.
  • Progestins — Progestins, synthetic hormones derived from naturally occurring progesterone, help promote the feminization process. They are taken orally through pills. 
  • Combination estrogen and progesterones — The combination of estrogen and progestins seeks a more balanced approach to feminization, counteracting some of the risks of estrogen alone. Additionally, it allows for further breast development and enhancement of other feminine features. Combination hormones are typically administered through oral pills.

FAQs

What is transgender hormone therapy, and why is it important?

Transgender hormone therapy involves the administration of hormones to align an individual's physical characteristics with their gender identity. For transgender individuals, this process is crucial for achieving a more authentic expression of their gender. It helps them fight issues like gender dysphoria and improve their overall well-being.

What happens if a man takes estrogen every day?

If a cisgender man takes transgender hormone pills like estrogen regularly, it can lead to the development of feminine secondary sexual characteristics. They may see changes such as breast growth, softer skin, and a different fat distribution. However, it's important to note that self-administering transgender drugs without professional guidance can have unpredictable and potentially harmful effects. For a successful transgender hormone therapy, please consult with a licensed endocrinologist.

Does estrogen change your face?

Yes, estrogen can contribute to changes in facial appearance during the feminizing process. These may include a softening of the skin, reduction in facial hair, and alterations in fat distribution.

Is feminizing hormone replacement therapy permanent?

Generally, yes, the effects are permanent. However, some changes, such as fat distribution and muscle mass reduction, may be reversible if hormone therapy is discontinued.

How long does hormone therapy for transgender individuals take?

The duration of hormone therapy varies widely. Changes typically begin within the first few months of the feminization or masculinization process, but the full effects may take one to two years or more. The process is gradual and continues over an extended period to allow for a more natural and sustainable transition.

How does one choose the right hormone therapy regimen?

The choice of hormones should be guided by healthcare professionals specializing in hormone replacement therapy for transgenders. It is highly personalized based on your desired features, health goals, and social preferences.


Are there risks associated with transgender hormone therapy?

Hormone replacement therapy for transgenders is generally safe under professional guidance. However, there are potential risks, including cardiovascular issues and changes in mood or mental health. Regularly monitor and communicate your condition with healthcare providers to address and mitigate these risks.

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